Wagenlehner F M E, Pilatz A, Naber K G, Perletti G, Wagenlehner C M, Weidner W
Department of Urology and Pediatric Urology, Justus-Liebig-University, Giessen, Germany.
Curr Med Chem. 2008;15(14):1412-27. doi: 10.2174/092986708784567699.
Bacterial urinary tract infections (UTI) are frequently found in the outpatient as well as in the nosocomial setting. The bacterial UTI can be stratified into uncomplicated and complicated UTI. Antibiotic resistance is continuously increasing in uncomplicated as well as complicated UTI. In uncomplicated UTI efforts are made to use antibiotic substances exclusively for this indication. In complicated UTI as broad spectrum antibiotics are increasingly used, the higher the antimicrobial resistance rates are reported. There are two predominant aims in the antimicrobial treatment of both uncomplicated and complicated UTI: 1.) rapid and effective response to therapy, prevention of complications and prevention of recurrence in the individual patient treated, and 2.) prevention of emergence of resistance to anti-infective agents in the microbial environment. The use of antibiotics has to keep up with the continuous change in antimicrobial resistance and the tailored needs in the individual patient. Antibiotic substances therefore need to become evaluated for each indication and continuously followed for clinical usage. The knowledge of structure-activity relationships of antimicrobial substances and bacterial resistance mechanisms to antibiotics help to use antibiotics better in daily routine and design new derivatives and substances. The aim of this review is to describe the chemistry and structure-activity relationships of current antibiotics and promising substances in development for the treatment of UTI.
细菌性尿路感染（UTI）在门诊和医院环境中都很常见。细菌性UTI可分为单纯性和复杂性UTI。单纯性和复杂性UTI中的抗生素耐药性都在持续增加。在单纯性UTI中，人们努力仅将抗生素用于该适应症。在复杂性UTI中，由于越来越多地使用广谱抗生素，报告的抗菌耐药率也越高。单纯性和复杂性UTI的抗菌治疗有两个主要目标：1.）对治疗做出快速有效的反应，预防并发症并防止接受治疗的个体患者复发；2.）防止微生物环境中对抗感染药物产生耐药性。抗生素的使用必须跟上抗菌耐药性的不断变化以及个体患者的特定需求。因此，需要针对每种适应症评估抗生素，并持续跟踪其临床使用情况。对抗菌物质的构效关系和细菌对抗生素的耐药机制的了解有助于在日常实践中更好地使用抗生素，并设计新的衍生物和物质。本综述的目的是描述当前用于治疗UTI的抗生素以及有前景的正在研发的物质的化学和构效关系。
